BROMFENAC BIOAVAILABILITY
Formulations and methods that provided enhanced bromfenac penetration into ocular tissue when topically administered, compared to the currently available BROMDAY™ formulation and method when topically administered. The formulations and methods did so while retaining the patient convenience of a once-daily administration and advantageously lowered the bromfenac concentration dosed to the patient.
1 . A method for treating a patient in need thereof with a bromfenac formulation comprising bromofenac as a free acid, the method comprising:
correlating bromfenac pH with bromfenac therapy but not bromfenac concentration by topically ocularly administering to the patient in need thereof the bromfenac formulation within a pH range between pH>6.0 and pH<8.3 and the bromfenac at a concentration between ≥0.02% w/v and ≤0.20% w/v,
wherein the pH range results in a bromfenac efficacy that is at least equal to an efficacy of bromfenac at 0.09% w/v and pH 8.3, and bromfenac is the only active.
2 . The method of claim 1 , wherein the bromfenac formulation contains >0.02% w/v and <0.20% bromfenac.
3 . The method of claim 1 , wherein the bromfenac formulation contains <0.09% w/v bromfenac.
4 . The method of claim 1 , wherein the bromfenac formulation is within a pH range between pH≥7.0 and ≤7.8.
5 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.0.
6 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.1.
7 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.2.
8 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.3.
9 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.4.
10 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.5.
11 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.6.
12 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.7.
13 . The method of claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.8.
14 . The method of claim 1 , wherein the bromfenac formulation further comprises tyloxapol, sodium sulfite, benzalkonium chloride, or a mixture thereof.
15 . The method of claim 1 , wherein the bromfenac formulation further comprises tyloxapol at a concentration of 0.01% w/v to 0.5% w/v, sodium sulfite, benzalkonium chloride at a concentration of ≤0.01% w/v, or a mixture thereof.
16 . A method for treating a patient in need thereof with bromfenac as a free acid, the method comprising:
(a) topically administering a first dose of bromfenac as the only active to an eye of the patient in need thereof, the bromfenac in a formulation where pH is >6.0 and <8.3 and where the bromfenac concentration is less than 0.09% w/v,
(b) administering at least a second dose of bromfenac to the eye of the patient in need thereof at a longer interval that exceeds twice a day administration of 0.09% w/v bromfenac at a pH>8.3, and
(c) assessing equal or greater efficacy in the patient administered bromfenac doses at the longer interval in the absence of bromfenac concentrations ≥0.09% w/v.
17 . The method of claim 16 , wherein the formulation is within a pH range between pH≥7.0 and ≤7.8.
18 . The method of claim 16 , wherein the formulation comprises 0.07% w/v bromfenac.
19 . The method of claim 16 , wherein the formulation further comprises tyloxapol, sodium sulfite, benzalkonium chloride, or a mixture thereof.
20 . The method of claim 16 , wherein the formulation further comprises tyloxapol at a concentration of 0.01% w/v to 0.5% w/v, sodium sulfite, benzalkonium chloride at a concentration of ≤0.01% w/v, or a mixture thereof.